HUP9900955A2 - 17-beta-cyclopropyl(amino/oxy) 4-aza steroids as active inhibitors of testosterone 5-alpha reductase and c17-20-lyase - Google Patents
17-beta-cyclopropyl(amino/oxy) 4-aza steroids as active inhibitors of testosterone 5-alpha reductase and c17-20-lyaseInfo
- Publication number
- HUP9900955A2 HUP9900955A2 HU9900955A HUP9900955A HUP9900955A2 HU P9900955 A2 HUP9900955 A2 HU P9900955A2 HU 9900955 A HU9900955 A HU 9900955A HU P9900955 A HUP9900955 A HU P9900955A HU P9900955 A2 HUP9900955 A2 HU P9900955A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- atom
- lyase
- testosterone
- cyclopropyl
- Prior art date
Links
- 108010029908 3-oxo-5-alpha-steroid 4-dehydrogenase Proteins 0.000 title 1
- 102000001779 3-oxo-5-alpha-steroid 4-dehydrogenase Human genes 0.000 title 1
- 150000000520 4-azasteroids Chemical class 0.000 title 1
- 125000002344 aminooxy group Chemical group [H]N([H])O[*] 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000001589 carboacyl group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 abstract 1
- -1 phenylthio, phenylsulfinyl Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
- C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
- C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines Containing Plant Substances (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
A találmány (I) általánős képletű vegyületekre és azők gyógyászatilagelfőgadható sóira vőnatkőzik, a képletben A jelentése őxigénatőm vagy-NH- csőpőrt, R1 jelentése hidrőgénatőm vagy alkilcsőpőrt, R2jelentése hidrőgénatőm, halőgénatőm, fenil-tiő-, fenil-szűlfinil- vagyfenil-szűlfőnil-csőpőrt, R3 jelentése hidrőgénatőm, halőgénatőm, akil-tiő-, alkil-szűlfinil- vagy alkil-szűlfőnil-csőpőrt, R4 jelentésehidrőgénatőm, alkilcsőpőrt vagy alkenilcsőpőrt, R5 jelentésehidrőgénatőm vagy alkilcsőpőrt, Z jelentése a) őxőcsőpőrt, b) kéthidrőgénatőm vagy egy a-hidrőgénatőm és egy b-helyettesítő, amelyetalkil-, alkenil-, hidrőxil-, alkanőil-őxi-, alkőxi-karbőnil-metil-,karbőxi-metil-, alkőxi-karbőnil-, karbőxil-, alkanőilcsőpőrt éshalőgénatőm közül választanak. ŕThe invention relates to compounds of the general formula (I) and their pharmaceutically acceptable salts, in the formula A is an oxygen atom or -NH atom, R1 is a hydrogen atom or an alkyl atom, R2 is a hydrogen atom, a halo atom, phenylthio, phenylsulfinyl or phenylsulfonyl , R3 Meaning Hydrően Venue, Fish Venue, Akil-Tiő, Alkyl-Sleeping or Alkyl-Szeklőnil Tube, R4 Meaning Hydhiden, Alkyl Tube or Alkenyl Tube, R5 Meaning Hydro an A-Broadcine Venue and a b-substituent selected from alkyl, alkenyl, hydroxy, alkanoyloxy, alkyloxycarbonylmethyl, carboxymethyl, carboxymethyl, carboxyl, alkanoyl, and halo. ŕ
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US60127896A | 1996-02-14 | 1996-02-14 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP9900955A2 true HUP9900955A2 (en) | 1999-07-28 |
| HUP9900955A3 HUP9900955A3 (en) | 2000-06-28 |
Family
ID=24406899
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU9900955A HUP9900955A3 (en) | 1996-02-14 | 1997-01-09 | 17-beta-cyclopropyl(amino/oxy) 4-aza steroids as active inhibitors of testosterone 5-alpha reductase and c17-20-lyase |
Country Status (17)
| Country | Link |
|---|---|
| EP (1) | EP0880540B1 (en) |
| JP (1) | JP2000505444A (en) |
| KR (1) | KR19990082543A (en) |
| CN (1) | CN1211256A (en) |
| AT (1) | ATE219100T1 (en) |
| AU (1) | AU710208B2 (en) |
| BR (1) | BR9708301A (en) |
| CA (1) | CA2244823A1 (en) |
| DE (1) | DE69713285T2 (en) |
| DK (1) | DK0880540T3 (en) |
| ES (1) | ES2178750T3 (en) |
| HU (1) | HUP9900955A3 (en) |
| IL (1) | IL125575A0 (en) |
| NO (1) | NO983724L (en) |
| NZ (1) | NZ327041A (en) |
| PT (1) | PT880540E (en) |
| WO (1) | WO1997030069A1 (en) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6187925B1 (en) | 1997-12-23 | 2001-02-13 | Merck & Co., Inc. | Intermediates and process for the synthesis of azasteroids |
| US6465445B1 (en) | 1998-06-11 | 2002-10-15 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
| US7005428B1 (en) | 1998-06-11 | 2006-02-28 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
| ATE440096T1 (en) * | 2000-12-08 | 2009-09-15 | Takeda Pharmaceutical | SUBSTITUTED THIAZOLE DERIVATIVES WITH 3-PYRIDYL GROUPS, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE |
| US7351698B2 (en) | 2003-05-07 | 2008-04-01 | Merck & Co., Inc. | Androgen receptor modulators and methods of use thereof |
| WO2009057795A2 (en) * | 2007-10-29 | 2009-05-07 | Takeda Pharmaceutical Company Limited | Pyrrolo [1,2-c] imidazole derivatives for use im the prophylaxis or treatment of cancer which is refractory to known cancer therapies |
| BRPI0920681A2 (en) * | 2008-10-28 | 2015-12-29 | Biomarin Pharm Inc | cyp17 decahidro-1h-indenoquinolinone and decahidro-3h-cyclopentafenantridinone inhibitors |
| US20110178065A1 (en) * | 2010-01-15 | 2011-07-21 | Biomarin Pharmaceutical Inc. | Novel cyp17 inhibitors |
| GB201102913D0 (en) | 2011-02-18 | 2011-04-06 | Univ Birmingham | Novel therapeutic |
| CN109438549B (en) * | 2018-12-13 | 2022-01-04 | 湖北葛店人福药业有限责任公司 | Method for preparing N-tert-butyl-3-oxo-4-aza-5 alpha-androstane-17 beta-formamide |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5264427A (en) * | 1992-01-29 | 1993-11-23 | Research Corporation Technologies, Inc. | 20-substituted pregnene derivatives and their use as androgen synthesis inhibitors |
| EP0641211A1 (en) * | 1992-05-21 | 1995-03-08 | Endorecherche Inc. | INHIBITORS OF TESTOSTERONE 5$g(a)-REDUCTASE ACTIVITY |
| US5486511A (en) * | 1993-05-25 | 1996-01-23 | Merrell Dow Pharmaceuticals Inc. | 4-amino-17β-(cyclopropyloxy)androst-4-en-3-one, 4-amino-17β-(cyclopropylamino)androst-4-en-3-one and related compounds as C17-20 lyase and 5α-reductase |
-
1997
- 1997-01-09 CA CA002244823A patent/CA2244823A1/en not_active Abandoned
- 1997-01-09 ES ES97901995T patent/ES2178750T3/en not_active Expired - Lifetime
- 1997-01-09 DE DE69713285T patent/DE69713285T2/en not_active Expired - Fee Related
- 1997-01-09 KR KR1019980706280A patent/KR19990082543A/en not_active Application Discontinuation
- 1997-01-09 NZ NZ327041A patent/NZ327041A/en unknown
- 1997-01-09 CN CN97192283A patent/CN1211256A/en active Pending
- 1997-01-09 AT AT97901995T patent/ATE219100T1/en not_active IP Right Cessation
- 1997-01-09 HU HU9900955A patent/HUP9900955A3/en unknown
- 1997-01-09 WO PCT/US1997/000469 patent/WO1997030069A1/en not_active Application Discontinuation
- 1997-01-09 DK DK97901995T patent/DK0880540T3/en active
- 1997-01-09 BR BR9708301A patent/BR9708301A/en not_active IP Right Cessation
- 1997-01-09 EP EP97901995A patent/EP0880540B1/en not_active Expired - Lifetime
- 1997-01-09 JP JP9529338A patent/JP2000505444A/en active Pending
- 1997-01-09 PT PT97901995T patent/PT880540E/en unknown
- 1997-01-09 IL IL12557597A patent/IL125575A0/en unknown
- 1997-01-09 AU AU15767/97A patent/AU710208B2/en not_active Ceased
-
1998
- 1998-08-13 NO NO983724A patent/NO983724L/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR19990082543A (en) | 1999-11-25 |
| PT880540E (en) | 2002-10-31 |
| NO983724D0 (en) | 1998-08-13 |
| DK0880540T3 (en) | 2002-10-07 |
| NO983724L (en) | 1998-10-13 |
| NZ327041A (en) | 1999-11-29 |
| BR9708301A (en) | 1999-08-03 |
| JP2000505444A (en) | 2000-05-09 |
| IL125575A0 (en) | 1999-03-12 |
| HUP9900955A3 (en) | 2000-06-28 |
| CA2244823A1 (en) | 1997-08-21 |
| EP0880540B1 (en) | 2002-06-12 |
| AU710208B2 (en) | 1999-09-16 |
| ATE219100T1 (en) | 2002-06-15 |
| ES2178750T3 (en) | 2003-01-01 |
| DE69713285D1 (en) | 2002-07-18 |
| WO1997030069A1 (en) | 1997-08-21 |
| CN1211256A (en) | 1999-03-17 |
| DE69713285T2 (en) | 2003-01-02 |
| AU1576797A (en) | 1997-09-02 |
| EP0880540A1 (en) | 1998-12-02 |
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